曲尼司特涂层支架的制备及体外释放度研究

Study on Release Profile of Tranilast From Tranilast-Eluting Stents in Vitro

目的探讨曲尼司特用于心脏涂层支架的可能性,建立曲尼司特涂层支架的制备方法,研究并考察影响释放动力学的因素。方法采用气体喷雾法制备曲尼斯特洗脱支架和洗脱不锈钢片,在37℃PBS中进行体外释放动力学研究,考察涂层各因素对释放动力学的影响。结果曲尼司特涂层支架中曲尼司特的释放速度随控释层厚度增加而减慢,随PLGA中GA比例的增加以及含药层中曲尼司特的含量增加而加速,优化的涂层支架可持续释放达35 d左右,释放度可达90%以上。结论曲尼司特洗脱支架体外释放动力学可以通过PLGA涂层的厚度,LA/GA比例以及含药层PLGA/药物重量比等因素加以调控。

OBJECTIVE To examine the feasibility of tranilast-eluting stent and various preparation conditions, and to investigate the factors that affect release kinetics.METHODS Trauilast-eluting stents and its substitute were prepared using air-brush.The release kinetics of tranilast from the stents was carried out by shaking in PBS buffer at 37℃, the release medium was sampled and subjected to HPLC measurement at scheduled date. RESULTS The release rate of tranilast was decreased by increasing the thickness of the controlling layer, and decreased with increasing the ration of LA/GA and the ratio of tranilast in drug-load layer, The optimized sample tranilast release lasted for 35 d, with accumulative release over 90%, CONCLUSION Tranilast can be coated on stent with PLGA, and released in a sustained manner. The release rates profile and duration can be controlled by the factors of the thickness of controlling layer, the ratio of LA/GA, the ratio of tranilast /PLGA and so on.